Glimekomb, pills 40+500mg, 60pcs

Composition

One tablet contains:  active ingredients: metformin hydrochloride in terms of 100% substance-500 mg, gliclazide in terms of 100% substance-40 mg; excipients: sorbitol, povidone, croscarmellose sodium, magnesium stearate.

Pharmacological action

Glimekomb is a combined hypoglycemic drug for oral use. Glimekomb® is a fixed combination of two oral hypoglycemic agents of the biguanide group and the group of sulfonylurea derivatives.

It has a pancreatic and extrapancreatic effect.

Gliclazide is a sulfonylurea derivative. It stimulates the secretion of insulin by the pancreas, increases the sensitivity of peripheral tissues to insulin. It stimulates the activity of intracellular enzymes-muscle glycogen synthetase. Restores the early peak of insulin secretion, reduces the time interval from the moment of food intake to the beginning of insulin secretion, reduces postprandial hyperglycemia.

In addition to influencing carbohydrate metabolism, it has an effect on microcirculation, reduces platelet adhesion and aggregation, delays the development of parietal thrombosis, normalizes vascular permeability and prevents the development of microthrombosis and atherosclerosis, restores the process of physiological parietal fibrinolysis, counteracts the increased reaction to vascular adrenaline in microangiopathies.

It slows down the development of diabetic retinopathy at the non-proliferative stage; with diabetic nephropathy, a significant decrease in proteinuria is noted against the background of long-term use. It does not lead to an increase in body weight, since it has a predominant effect on the early peak of insulin secretion and does not cause hyperinsulinemia; it contributes to weight loss in obese patients with an appropriate diet.

Metformin belongs to the biguanide group. Reduces the concentration of glucose in the blood by inhibiting gluconeogenesis in the liver, reducing the absorption of glucose from the gastrointestinal tract and increasing its utilization in tissues. Reduces the concentration of triglycerides, cholesterol and LDL in the blood serum (determined on an empty stomach) and does not change the concentration of lipoproteins of other densities. Helps to stabilize or reduce body weight. In the absence of insulin in the blood, the therapeutic effect is not manifested. It does not cause hypoglycemic reactions. Improves the fibrinolytic properties of blood by suppressing the tissue-type activator inhibitor profibrinolysin (plasminogen).

Pharmacokinetics

Gliclazide

Suction and distribution

After oral use, absorption is high. When taken at a dose of 40 mg, Cmax in blood plasma is reached in 2-3 hours and is 2-3 mcg / ml. Binding to plasma proteins is 85-97%.

Metabolism and elimination

It is metabolized in the liver. T1 / 2 – 8-20 hours It is mainly excreted in the form of metabolites by the kidneys-70%, through the intestines-12%.

No clinically significant changes in pharmacokinetic parameters were observed in elderly patients.

Metformin

Suction and distribution

After oral use, the absorption is 48-52%. It is rapidly absorbed from the gastrointestinal tract. Absolute bioavailability (on an empty stomach) is 50-60%. Cmax in blood plasma is reached in 1.81-2.69 hours and does not exceed 1 mcg / ml. Food intake reduces plasma Cmax by 40% and slows its achievement by 35 minutes. Binding to plasma proteins is insignificant. Metformin is able to accumulate in red blood cells.

Excretion

T1 / 2 is 6.2 h. It is excreted by the kidneys, mainly in unchanged form (glomerular filtration and tubular secretion) and through the intestine (up to 30%).

Indications

Type 2 diabetes mellitus with ineffectiveness of diet therapy, exercise and previous therapy with metformin or gliclazide.

Replacement of previous therapy with two drugs (metformin and gliclazide) in patients with type 2 diabetes mellitus with stable and well-controlled blood glucose levels.

Contraindications

• diabetes mellitus type 1 (insulin-dependent);
• diabetic ketoacidosis;
• diabetic precoma, diabetic coma;
• hypoglycemia;
• severe renal dysfunction;
• acute conditions that can lead to a change in kidney function, dehydration, severe infection, shock;
• acute or chronic diseases that are accompanied by hypoxia of tissues: cardiac failure, respiratory failure, recent myocardial infarction, shock;
• hepatic impairment;
• porphyria;
• pregnancy;
• lactation (breastfeeding);
• simultaneous reception of miconazole;
• state requiring insulin, including infectious diseases, major surgery, trauma, extensive burns;
• chronic alcoholism;
• acute alcohol intoxication,
• lactic acidosis (including history);
• application of at least 48 hours prior to and within 48 hours after the radioisotope or radiological examinations with use of iodinated contrast agents;
• adherence to a reduced-calorie diet (less than 1000 cal/day);
• hypersensitivity to the components of the drug;
• hypersensitivity to other sulfonylureas.

It is not recommended to use the drug in patients over 60 years of age who perform heavy physical work, which is associated with an increased risk of lactic acidosis.

With caution, the drug should be used for fever syndrome, adrenal insufficiency, hypofunction of the anterior pituitary gland, diseases of the thyroid gland with impaired function.

Side effects

From the endocrine system:  hypoglycemia (in case of violation of the dosage regimen and inadequate diet) – headache, fatigue, hunger, increased sweating, sudden weakness, palpitations, dizziness, impaired coordination of movements, temporary neurological disorders; with the progression of hypoglycemia, loss of self-control, loss of consciousness is possible.

From the side of metabolism:  in some cases – lactic acidosis (weakness, myalgia, respiratory disorders, drowsiness, abdominal pain, hypothermia, decreased blood pressure, bradyarrhythmia).

From the digestive system:  dyspepsia (nausea, diarrhea, a feeling of heaviness in the epigastrium, a “metallic” taste in the mouth), decreased appetite (the severity of these reactions decreases when taking the drug during meals); rarely-hepatitis, cholestatic jaundice (drug withdrawal is required), increased activity of hepatic transaminases, alkaline phosphatase.

From the hematopoietic system:  rarely-inhibition of bone marrow hematopoiesis (anemia, thrombocytopenia, leukopenia).

Allergic reactions:  pruritus, urticaria, maculopapular rash.

Other services:  visual impairment.

In cases of side effects, the dose should be reduced or the drug should be temporarily discontinued.

Common side effects of Sulfonylurea derivatives:  erythropenia, agranulocytosis, hemolytic anemia, pancytopenia, allergic vasculitis, life-threatening liver failure.

Interaction

Increased hypoglycemic effect of Glimekomb is observed when used concomitantly with ACE inhibitors (captopril, enalapril), histamine H2-receptor blockers (cimetidine), antifungal drugs (miconazole, fluconazole), NSAIDs (phenylbutazone, azapropazone, oxifenbutazone), fibrates (clofibrate, bezafibrate), anti-tuberculosis drugs (ethionamide), salicylates, coumarin-type anticoagulants, anabolic steroids, beta-blockers, MAO inhibitors, long-acting sulfonamides, with cyclophosphamide, chloramphenicol, fenfluramine, fluoxetine, guanethidine, pentoxifylline, tetracycline, theophylline, tubular secretion blockers, reserpine, bromocriptine, disopyramide, pyridoxine, with other hypoglycemic drugs (including acarbose, biguanides, insulin), allopurinol, oxytetracycline.

A decrease in the hypoglycemic effect of Glimekomb is observed when used simultaneously with barbiturates, corticosteroids, adrenomimetics (epinephrine, clonidine), antiepileptic drugs (phenytoin), slow calcium channel blockers, carbonic anhydrase inhibitors (acetazolamide), thiazide diuretics, chlortalidone, furosemide, triamterene, asparaginase, baclofen, danazol, diazoxide, isoniazid, morphine, ritodrin, salbutamol, terbutaline, glucagon, rifampicin, thyroid hormones, lithium salts, high-dose nicotinic acid, chlorpromazine, oral contraceptives and estrogens.

Increases the risk of ventricular extrasystole due to cardiac glycosides.

Medications that inhibit bone marrow hematopoiesis increase the risk of myelosuppression.

Ethanol increases the likelihood of developing lactic acidosis.

Pharmacokinetic interaction

Metformin reduces plasma Cmax and furosemide T1 / 2 by 31 and 42.3%, respectively.

Furosemide increases the Cmax of metformin by 22%.

Nifedipine increases absorption, increases Cmax in blood plasma, slows down the elimination of metformin.

Cationic drugs (amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene, and vancomycin) secreted in the tubules compete for tubular transport systems and, with prolonged therapy, can increase the Cmax of metformin in blood plasma by 60%.

How to take it, course of use and dosage

The drug Glimekomb is used orally, during or immediately after a meal. The dose of the drug is determined by the doctor individually for each patient, depending on the blood glucose level.

Usually, the initial dose is 1-3 tablets per day with a gradual selection of the dose until stable compensation of the disease is achieved.

Usually the drug is taken 2 times a day (in the morning and in the evening). The maximum daily dose is 5 tablets.

Overdose

Symptoms: lactic acidosis (because the drug contains metformin), hypoglycemia are possible.

Treatment: if you experience symptoms of lactic acidosis, you should stop taking the drug. Lactic acidosis is a condition that requires urgent medical attention; treatment is carried out in a hospital. The most effective method of treatment is hemodialysis.

With mild or moderate hypoglycemia, glucose (dextrose) or a sugar solution is taken orally. In case of severe hypoglycemia (loss of consciousness), a 40% dextrose (glucose) solution or glucagon is administered intravenously, intramuscularly or subcutaneously. After regaining consciousness, the patient should be given food rich in carbohydrates, in order to avoid the re-development of hypoglycemia.

Composition

Tablet Form of production

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C.

Shelf life

2 years

Active ingredient

Gliclazide, Metformin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Type 2 Diabetes